Synthesis and binding monitoring of a new nanomolar PAMAM-based matrix metalloproteinases inhibitor (MMPIs)

新型纳摩尔 PAMAM 基基质金属蛋白酶抑制剂 (MMPI) 的合成及结合监测

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作者:Linda Cerofolini, Veronica Baldoneschi, Elisa Dragoni, Andrea Storai, Marianna Mamusa, Debora Berti, Marco Fragai, Barbara Richichi, Cristina Nativi

Abstract

Dendrimers are efficient drug delivery systems particularly useful in ocular diseases. In particular, low generation PAMAM dendrimers are non-toxic and non-immunogenic and they provide an enhancement of the residence time of drugs in the eyes. In this context, the synthesis of the PAMAM-based matrix metalloproteinases inhibitor 5, is reported. In particular, we demonstrated that 5 strongly binds (18.0nM±2.5nM) MMP-9, the most relevant MMP responsible of ocular surface damages in induced dry eyes syndrome (DES).

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